Introduction: Because of their important roles in disease and excellent 'druggability', kinases
have become the second largest drug target family. The great success of the BCR-ABL …

Protein kinases have emerged as one of the most frequently targeted families of proteins in
drug discovery. While the development of small-molecule inhibitors that have the potency …

In this article, we are reviewing the molecular mechanisms that lead to kinase inhibitor
resistance. As the oncogenic BCR-ABL kinase is the target of the first approved small …

Mechanisms of resistance to the tyrosine kinase inhibitor (TKI) imatinib had been modeled in
vitro even prior to the first reports of clinical resistance in patients with chronic myeloid …

Since the introduction of imatinib mesylate (IM) for the treatment of chronic myeloid leukemia
(CML), impressive clinical responses have been observed in the majority of patients in …

Selective inhibition of protein tyrosine kinases is gaining importance as an effective
therapeutic approach for the treatment of a wide range of human cancers. However, as …

Resistance against tyrosine kinase inhibitors (TKIs) represents a relevant clinical problem in
treatment of chronic myelogenous leukemia (CML). On the basis of their activity against the …

Although only 5000 new cases of chronic myeloid leukemia (CML) were seen in the United
States in 2009, this neoplasm continues to make scientific headlines year-after-year …

The use of small molecules became one key cornerstone of targeted anti-cancer therapy.
Among them, tyrosine kinase inhibitors (TKIs) are especially important, as they were the first …

Imatinib, a specific small molecule inhibitor of the Abl kinase, has become the standard drug
therapy for chronic myelogenous leukemia in all phases. More than 80% of newly …